In vitro suppression of HIV-1 replication by ajoene [(e)-(z)-4,5,9-trithiadodeca-1,6,11-triene-9 oxide].
Studies were performed to establish whether synthetic ajoene exhibited differential inhibitory activity against human immunodeficiency virus (HIV)-1 (IIIB) and to clarify the mechanism of its antiviral effects. Our results demonstrate that ajoene protected acutely infected Molt-4 cells against HIV-1 and blocked further destruction of CD4 T-cells in vitro. Ajoene showed dose-dependent inhibition, with 50% cytotoxic concentration (CTC50%) and 50% effective inhibitory concentration (EIC50%) values of 1.88 microM and about 0.35 microM, respectively, when the test compound was added before or after HIV-1 infection and incubation carried out at 37 degrees C for 4 days. Ajoene proved relatively more active than dextran sulfate in blocking HIV-1 virus-cell attachment. The mode of anti-HIV action of ajoene can be ascribed to the inhibition of early events of viral replication, particularly virus adsorption.
Walder
R
R
Centro de Microbiología y Biología Celular, Instituto Venezolano de Investigaciones Científica, Caracas, Venezuela.
Kalvatchev
Z
Z
Garzaro
D
D
Barrios
M
M
Apitz-Castro
R
R
D000327:Adsorption; D000998:Antiviral Agents / Q000494:pharmacology*; D003470:Culture Media; D004220:Disulfides / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004355:Drug Stability; D015497:HIV-1 / Q000502:physiology*; D066298:In Vitro Techniques; D010936:Plant Extracts / Q000494:pharmacology*; D013454:Sulfoxides; D014779:Virus Replication / Q000187:drug effects*
D000998:Antiviral Agents; D003470:Culture Media; D004220:Disulfides; D010936:Plant Extracts; D013454:Sulfoxides; C048980:ajoene